5-HT3A | 5-HT3A/C | 5-HT3A/E | 5-HT3A/Ea | 5-HT3A | 5-HT3A/D | |
---|---|---|---|---|---|---|
Agonist pEC50 [(mean EC50) μM] | ||||||
5-HT | 5.75 ± 0.03 (1.81) | 5.75 ± 0.04 (1.79) | 5.78 ± 0.03 (1.66) | 5.76 ± 0.03 (1.76) | 5.70 ± 0.03 (2.02) | |
mCPBG | 5.82 ± 0.03 (1.52) | 5.80 ± 0.03 (1.61) | 5.86 ± 0.04 (1.40) | 5.74 ± 0.04 (1.83) | 5.72 ± 0.03 (1.94) | |
Antagonist pIC50 [(mean IC50) nM] | ||||||
Ondansetron | 9.23 ± 0.06 (0.63) | 9.34 ± 0.15 (0.52) | 9.22 ± 0.07 (0.63) | 9.35 ± 0.06 (0.46) | 9.00 ± 0.02 (1.01) | 8.88 ± 0.04 (1.33) |
Azasetron | 9.12 ± 0.01 (0.77) | 9.09 ± 0.03 (0.83) | 9.05 ± 0.04 (0.91) | 9.15 ± 0.07 (0.74) | 8.96 ± 0.03 (1.11) | 8.87 ± 0.06 (1.39) |
Emax [% of 5-HT3A + ss Emax] | 100.00 ± 15.20 | 70.72 ± 10.61* | 144.32 ± 22.82** | 43.87 ± 5.59** | 100.00 ± 6.95 | 145.76 ± 10.22** |
Significant differences (repeated ANOVA followed by Dunnett's post test) compared with homopentameric 5-HT3A receptors: *p < 0.05, and **p < 0.01.